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In order to get novel EGFR inhibitors exerting more potency in tumor hypoxia than in normoxia.Methods
A series of 4-[(2-nitroimidazole-1
H-alkyloxyl)
aniline]-quinazolines were designed and synthesized, and their in vitro cytotoxicity and EGFR
A series of aniline mustards with a wide range of electron-donating and -withdrawing substituents in the 3- and 4-positions has been synthesized and evaluated for cytotoxicity in cell culture to examine the potential of using nitro group deactivated nitrogen mustards for the design of novel
To elucidate the role of N-phenylhydroxylamine (PHA, N-hydroxylated metabolite of aniline) in the selective toxicity of aniline to the spleen, dose-dependent studies were conducted with PHA in rats. Male Sprague-Dawley rats were given four doses each (1 dose/day) of 0.025, 0.05, 0.1, or 0.2 mmol/kg
The hepatic drug metabolising enzymes activity has been studied in rats exposed to acute hypoxia alone or along with supplementation of single dose of 10 000 I.U. Vitamin A. Hypoxic stress reduces the activities of cytochrome P-450, cytochrome c-reductase and aniline hydroxylase. Administration of
Influence of hypoxia (0.029 MPa, I h) followed by hyperoxia (0.2 MPa, I h) on microsomal oxidation and lipoperoxidation was studied in rat liver and lungs. Distinct increase of cytochrome P-450 catalytic activity with amidopyrine and benzo-a-pyrene as substrates of the I type was found after
Content and catalytic activity of cytochrome P-450 were studied using amidopyrine as a substrate of the I type and aniline as a substrate of the II type. In hypoxia content of cytochrome P-450 and metabolism of amidopyrine were increased, while the enzyme content and the substrate metabolism were
This review describes histopathologic observations made with both light and electron microscopy using both conventional staining techniques and histochemistry. Several conditions are analyzed: Ischemic cell change; delayed neuronal death; selective vulnerability. The histopathologic support for the
The hepatic MFO activity has been studied in rats exposed to acute hypoxia given single dose of ethanol (3 g/kg body weight) alone or along with 10,000 I.U. of vitamin A. The cytochrome P-450 was found to be depressed on ethanol administration in rats. Hypoxic exposure of rats given ethanol with or
Arginine, preadministered intraperitoneally at a dose of 120 mg per 100 g of body mass before hypoxia, decreased content of diene conjugates by 42-64% and Schiff bases by 7-15% in rat liver and testicular microsomal membranes as compared with control rats nontreated with arginine. Under these
The increase of cytochrome P-450 by 34% and its catalytic activity with substrate amidopyrine by 57% as compared with control has been shown under hypoxia (0.029 MPa, 1 h). Hyperoxia (0.2 MPa, 1 h) increases the metabolism of amidopyrine by 148%, benzo[a]pyrene by 158% and aniline by 114% and
Sixteen novel epidermal growth factor receptor (EGFR)/vascular endothelial growth factor (VEGF)-2 inhibitors (nitroimidazole-substituted 4-anilinoquinazoline derivatives (16a-p)) were designed and prepared via the introduction of a nitroimidazole group in the piperidine side chain and modification
Tyrosine kinase inhibitors (TKIs) have achieved substantial clinical effects for cancer treatment while causing a number of adverse effects. Since hypoxia is an intrinsic difference between solid tumor and healthy tissues, one strategy to overcome the adverse effects of TKIs is to enhance the
A 16-year-old girl working in a paint and dye-casting factory of aniline dyes presented to the emergency with cyanosis, fever and altered sensorium. She had been diagnosed as a case of malaria and treated with chloroquine elsewhere. At admission, her saturation was 79%, which did not improve despite
It was shown that animals divided into groups with respect to the initial sensitivity (low and high resistance) to hypoxia (lack of oxygen in air) differ by their liver monooxygenase enzyme complex reaction to the model acute hypoxia. Low-resistant rats exhibited an increase in cytochromes P-450 and